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br Presenilins in protein trafficking
2022-03-29

Presenilins in protein trafficking, proteolysis and degradation An obvious explanation for the role of presenilins and γ-secretase in protein trafficking and degradation is that many reported γ-secretase substrates are functionally involved in protein transport. For example, members of the mammal
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br ACKNOWLEDGMENTS br Introduction Odorant receptors
2022-03-29

ACKNOWLEDGMENTS Introduction Odorant receptors (ORs) are the largest subfamily of G protein-coupled receptors (GPCRs) and are mainly expressed by olfactory sensory neurons in the nose for the detection of various odorants [1]. However, more recent reports suggest that ORs are also expressed an
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Herein we report the discovery of AM AM maintains
2022-03-29

Herein, we report the discovery of AM-3189 (). AM-3189 maintains the in vivo efficacy of AMG 837 while displaying a superior pharmacokinetic profile and minimal CNS exposure. As we reported previously, activity on the GPR40 receptor varies significantly with substitution at the β-carbon relative to
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Several observations about structure activity relationships
2022-03-28

Several observations about structure–activity relationships can be made from this series, including that: (1) all lead compounds are NSAIDs of the 2-arylpropionic TDZD-8 class, (2) analogues with -oriented aryl substituents showed the best inhibition of FAAH, and (3) replacing the ether linkage of f
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Not only does G a GLP complex appear to play
2022-03-28

Not only does G9a/GLP complex appear to play a role (albeit a seemingly conflicting one) in LTP maintenance, it may also be involved in long-term depression (LTD) (). At hippocampal CA1 synapses, LTD can be induced by pharmacological or synaptic stimulation of Group 1 metabotropic glutamate receptor
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In the present study we focused on a role
2022-03-28

In the present study, we focused on a role of the C-terminal segment in GCAP2 using two chimeric proteins, in which the C-terminal segment of GCAP2 was either replaced by the corresponding sequence of recoverin (chimera GR) or transferred into recoverin (chimera RG). We have monitored Ca-dependent
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A number of in vivo studies
2022-03-28

A number of in vivo studies have investigated the antitumor activity of distinct GSK-3 inhibitors in a variety of cancer cell line-derived tumor xenograft models [14], [21], [22], [24], [33], [39], [40]. These studies utilized toolkit GSK-3 inhibitors as monotherapies. Although inhibition of tumor g
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br Regulation of gonadotropins by GnRH GnRH is
2022-03-28

Regulation of gonadotropins by GnRH GnRH is released from the hypothalamus, and its release pattern is known to be pulsatile. That is, the pulse frequency and amplitude of GnRH release vary physiologically during reproductive cycles in females, and differentially stimulate the production and rele
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Due to the therapeutic potential of
2022-03-28

Due to the therapeutic potential of GlyT1 inhibitors, numerous drug screening campaigns have been started - and are still going on - which aimed at the identification of compounds with biological activity at or affinity for this drug target. For characterization of biological activity at GlyT1, tran
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br Materials and methods br
2022-03-28

Materials and methods Results Discussion All the UDG superfamily glycosylases examined here, UDG, SMUG1, TDGFL, and TDG82−308, are capable of completely converting U-containing duplex substrates to product, though at different rates. Under STO conditions, kobs reflects the slowest kinetic s
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br Conclusion In summary a series of
2022-03-28

Conclusion In summary, a series of novel GPR40 agonists bearing phenylpropiolic HJC 0350 motif with favorable metabolic stability were prepared and evaluated for their activities as GPR40 agonists. Among them, compound 9 was identified as a structurally distinct GPR40 agonist possessing potent ac
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Recent studies suggested that non coding RNAs participate in
2022-03-28

Recent studies suggested that non-coding RNAs participate in the modulation of Glut1 expression. For instance, the lncRNA NBR2-Glut1 axis was suggested to modulate cancer cell sensitivity to phenformin [37]. In renal carcinoma, miR-1291 is involved in the regulation of Glut1 Lapatinib [38]. Therefo
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br Materials and methods br Results br
2022-03-26

Materials and methods Results Discussion BTB, as a necessary structure for the spermatogenic epithelium, provides an important internal environmental for spermatogenesis and its disruption leads to male infertility (Qiu et al., 2016). GJs and TJs which are mainly components of BTB play esse
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Notwithstanding the functioning of galaninergic system may b
2022-03-26

Notwithstanding, the functioning of galaninergic system may be even more complex (Fuxe et al., 2012). Some studies present evidence that GAL2 receptors might form heteroreceptor complexes with neuropeptide Y1 receptors in Efavirenz of amygdala (Narváez et al., 2015a), DRN (Díaz-Cabiale et al., 2011
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Pregnenolone Carbonitrile mg In the present study the
2022-03-26

In the present study, the relative mRNA Pregnenolone Carbonitrile mg levels of CsLCCH3 and Cs8916 subunits in the egg were the highest, which were consistent with those of LsLCCH3 and Ls8916 from L. striatellus (Wei et al., 2017b) and were also similar to CsRDLs (Sheng et al., 2018; Meng et al., 201
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